Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.
Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo profile of analog 20 is described.
Fan
Junfa
J
Sunesis Pharmaceuticals, 341 Oyster Point Blvd, South San Francisco, CA 94080, USA. jfan@sunesis.com
Fahr
Bruce
B
Stockett
David
D
Chan
Erica
E
Cheeti
Sravanthi
S
Serafimova
Iana
I
Lu
Yafan
Y
Pham
Phuongly
P
Walker
Duncan H
DH
Hoch
Ute
U
Choong
Ingrid C
IC
D000818:Animals; D020650:Combinatorial Chemistry Techniques; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors*; D007540:Isonipecotic Acids / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D010080:Oxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D007540:Isonipecotic Acids; C484864:N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide; D010080:Oxazoles; D013844:Thiazoles; D051357:Cyclin-Dependent Kinase 2